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1. 发明申请

WO2019094319A1 PYRROLOPYRAZINE DERIVATIVES AS ALPHA V INTEGRIN INHIBITORS 审中-公开
公开(公告)号：WO2019094319A1
公开(公告)日：2019-05-16
申请号：PCT/US2018/059157
申请日：2018-11-05
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： ZHAO, Guohua , MIGNONE, James
IPC分类号： C07D487/04 , A61P35/00 , A61K31/00
CPC分类号： C07D487/04 , A61P35/00
摘要： The disclosure relates to compounds of formula I: Formula I which inhibit α v-containing integrins, and includes pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of α V-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders.

2. 发明申请

WO2018089360A1 PYRROLE AMIDES AS ALPHA V INTEGRIN INHIBITORS 审中-公开
标题翻译：吡咯酰胺作为ALPHA V INTEGRIN抑制剂
公开(公告)号：WO2018089360A1
公开(公告)日：2018-05-17
申请号：PCT/US2017/060392
申请日：2017-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： ZHAO, Guohua , MIGNONE, James
IPC分类号： C07D471/04 , A61K31/4375 , A61P11/00
摘要： The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are inhibitors to α v -containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αv-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
摘要翻译：本发明提供式（I）的化合物或其立体异构体，互变异构体或药学上可接受的盐或溶剂合物，其中所有变量如本文所定义。这些化合物是含有αvβ1整联蛋白的抑制剂。本发明还涉及包含这些化合物的药物组合物以及通过使用所述化合物治疗与包含αv的整联蛋白失调相关的疾病，病症或病症（例如病理性纤维化，移植排斥，癌症，骨质疏松症和炎性病症）的方法和药物组合物。

3. 发明申请

WO2015191681A2 SUBSTITUTED PYRIDINONES AS MGAT2 INHIBITORS 审中-公开
标题翻译：取代的吡啶酮作为MGAT2抑制剂
公开(公告)号：WO2015191681A2
公开(公告)日：2015-12-17
申请号：PCT/US2015/035054
申请日：2015-06-10
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DEVASTHALE, Pratik , MOORE, Fang , MIGNONE, James , WANG, Wei
CPC分类号： A61K31/4418 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D213/74 , C07D213/80 , C07D213/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/14
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
摘要翻译：本发明提供式（I）的化合物或其立体异构体，互变异构体，药学上可接受的盐，多晶型物或溶剂化物，其中所有变量如本文所定义。这些化合物是可用作药物的单酰基甘油酰基转移酶2型（MGAT2）抑制剂。

4. 发明申请

WO2010042674A1 PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：吡咯酮梅兰宁浓缩HORMONE RECEPTOR-1 ANTAGONISTS
公开(公告)号：WO2010042674A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/059918
申请日：2009-10-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , ZHAO, Guohua , WASHBURN, William N. , MIGNONE, James
发明人： ZHAO, Guohua , WASHBURN, William N. , MIGNONE, James
IPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/407 , A61P3/00
CPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R 1 , Formula Ia, R 4 , R 5 , Formula Ib, R 3 , R 3a , W, D, R 2a , R 2b and R 2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.
摘要翻译：本申请提供化合物，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式，其中R1，式Ia，R4，R5，式Ib，R3，R3a，W，D，R2a，R2b和R2c被定义于此。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。最后，本申请提供了通过施用治疗有效剂量的化合物来治疗患有MCHR-1调节的疾病或病症例如肥胖症，糖尿病，抑郁症，焦虑或肠道炎症的患者的方法，一级方程式

5. 发明授权

EP2346860B1 PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 有权
标题翻译：用于黑色素浓缩激素的REZEPTOREPTORS 1吡咯酮作为拮抗剂
公开(公告)号：EP2346860B1
公开(公告)日：2012-09-19
申请号：EP09793348.5
申请日：2009-10-08
申请人： Bristol-Myers Squibb Company
发明人： ZHAO, Guohua , WASHBURN, William N. , MIGNONE, James
IPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/407 , A61P3/00
CPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04

6. 发明公开

EP2346860A1 PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 有权
标题翻译：用于黑色素浓缩激素的REZEPTOREPTORS 1吡咯酮作为拮抗剂
公开(公告)号：EP2346860A1
公开(公告)日：2011-07-27
申请号：EP09793348.5
申请日：2009-10-08
申请人： Bristol-Myers Squibb Company
发明人： ZHAO, Guohua , WASHBURN, William N. , MIGNONE, James
IPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/407 , A61P3/00
CPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R
1 , Formula Ia, R
4 , R
5 , Formula Ib, R
3 , R
3a , W, D, R
2a , R
2b and R
2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.

7. 发明公开

EP3707142A1 PYRROLOPYRAZINE DERIVATIVES AS ALPHA V INTEGRIN INHIBITORS 有权
公开(公告)号：EP3707142A1
公开(公告)日：2020-09-16
申请号：EP18804882.1
申请日：2018-11-05
申请人： Bristol-Myers Squibb Company
发明人： ZHAO, Guohua , MIGNONE, James
IPC分类号： C07D487/04 , A61P35/00 , A61K31/00

8. 发明公开

EP3154944A2 SUBSTITUTED PYRIDINONES AS MGAT2 INHIBITORS 有权
标题翻译：替补吡虫啉ALS MGAT2-INHIBITOREN
公开(公告)号：EP3154944A2
公开(公告)日：2017-04-19
申请号：EP15795011.4
申请日：2015-06-10
申请人： Bristol-Myers Squibb Company
发明人： DEVASTHALE, Pratik , MOORE, Fang , MIGNONE, James , WANG, Wei
IPC分类号： C07D213/82 , C07D401/14 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , A61K31/4412 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61P1/16 , A61P3/00 , A61P9/00 , A61P27/06
CPC分类号： A61K31/4418 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D213/74 , C07D213/80 , C07D213/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/14
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
摘要翻译：本发明提供式（I）的化合物：或其立体异构体，互变异构体，药学上可接受的盐，多晶型物或溶剂化物，其中所有变量如本文所定义。这些化合物是可用作药物的单酰基甘油酰基转移酶2型（MGAT2）抑制剂。

9. 发明授权

EP3154944B1 SUBSTITUTED PYRIDINONES AS MGAT2 INHIBITORS 有权
标题翻译：作为MGAT2抑制剂的取代的吡啶酮
公开(公告)号：EP3154944B1
公开(公告)日：2018-03-14
申请号：EP15795011.4
申请日：2015-06-10
申请人： Bristol-Myers Squibb Company
发明人： DEVASTHALE, Pratik , MOORE, Fang , MIGNONE, James , WANG, Wei
IPC分类号： C07D213/82 , C07D401/14 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , A61K31/4412 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61P1/16 , A61P3/00 , A61P9/00 , A61P27/06
CPC分类号： A61K31/4418 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D213/74 , C07D213/80 , C07D213/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/14
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

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